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1mg | ||
2mg | ||
5mg | ||
10mg | ||
25mg |
Purity: ≥98%
Pam3CSK4 is a novel and potent TLR1/2 (toll-like receptor 1/2) agonist with an EC50 of 0.47 ng/mL for human TLR1/2. Pam3CSK4 is able to attenuate inflammatory responses caused by systemic infection of methicillin-resistant Staphylococcus aureus in mice. Combination of C and Pam3CSK4 enhances activation of B cells in vitro and boosts antibody responses to protein vaccines in vivo.
ln Vitro |
Pam3CSK4 is a triacylated lipopeptide-recognizing TLR1/2 heterodimer [1]. Methicillin-resistant Staphylococcus aureus is more susceptible to the antibacterial activity of neutrophils elicited by granulocyte macrophage colony-stimulating factor (GM-CSF) when treated with 1 μg/mL of Pam3CSK4 [2].
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ln Vivo |
In newborn mice, Pam3CSK4 (5 mg/kg; i.p.; once daily for 9 days) alters the weights of the liver, spleen, and brain [3].
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Animal Protocol |
Animal/Disease Models: timely mated pregnant C57BL/6 wild-type mice; B6.129-Tlr2tm1Kir/J (TLR2 deficient) mice [3]
Doses: 5 mg/kg Route of Administration: intraperitoneal; one time/day, Results lasting 9 days: After repeated dosing from postnatal (PND3) to PND11, brain weight diminished compared to animals treated with endotoxin-free saline at PND12. At PND12, cerebral gray matter, forebrain white matter, and cerebellum molecular layer volumes diminished, while spleen and liver weights increased. |
References |
[1]. Irvine KL, et al. The molecular basis for recognition of bacterial ligands at equine TLR2, TLR1 and TLR6. Vet Res. 2013 Jul 4;44:50.
[2]. Chen Y, et al. TLR2 agonist Pam3CSK4 enhances the antibacterial functions of GM-CSF induced neutrophils to methicillin-resistant Staphylococcus aureus. Microb Pathog. 2019 May;130:204-212. [3]. Du X, et al. Systemic stimulation of TLR2 impairs neonatal mouse brain development. PLoS One. 2011 May 6;6(5):e19583. |
Molecular Formula |
C81H159CL3N10O13S
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Molecular Weight |
1510.22954
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CAS # |
112208-00-1
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Related CAS # |
Pam3CSK4 TFA;112208-01-2;Pam3CSK4 trihydrochloride;112208-04-5
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Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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SMILES |
O=C(N[C@@H](CCCCN)C(N[C@@H](CCCCN)C(N[C@@H](CCCCN)C(N[C@@H](CCCCN)C(O)=O)=O)=O)=O)[C@H](CO)N(C([C@@H](NC(CCCCCCCCCCCCCCC)=O)CS)=O)CC(OC(CCCCCCCCCCCCCCC)=O)COC(CCCCCCCCCCCCCCC)=O.
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InChi Key |
LBBMJOSYFJWKTM-PXSLIBMESA-N
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InChi Code |
InChI=1S/C81H156N10O13S.3ClH/c1-4-7-10-13-16-19-22-25-28-31-34-37-40-55-73(93)86-71(65-105)80(100)91(62-66(104-75(95)57-42-39-36-33-30-27-24-21-18-15-12-9-6-3)64-103-74(94)56-41-38-35-32-29-26-23-20-17-14-11-8-5-2)72(63-92)79(99)89-69(53-45-49-60-84)77(97)87-67(51-43-47-58-82)76(96)88-68(52-44-48-59-83)78(98)90-70(81(101)102)54-46-50-61-85/h66-72,92,105H,4-65,82-85H2,1-3H3,(H,86,93)(H,87,97)(H,88,96)(H,89,99)(H,90,98)(H,101,102)3*1H/t66?,67-,68-,69-,70-,71-,72-/m0.../s1
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Chemical Name |
Palmitoyl-Cys((RS)-2,3-di(palmitoyloxy)-propyl)-Ser-Lys-Lys-Lys-Lys-OH trihydrochloride
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Synonyms |
Pam3CSK4 Pam3CSK4 HCl Pam3CSK4 Pam3-Cys-Ser-Lys-Lys-Lys-Lys
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HS Tariff Code |
2934.99.9001
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80: Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 :Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400  (Please use freshly prepared in vivo formulations for optimal results.) |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 0.6622 mL | 3.3108 mL | 6.6215 mL | |
5 mM | 0.1324 mL | 0.6622 mL | 1.3243 mL | |
10 mM | 0.0662 mL | 0.3311 mL | 0.6622 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.